| Chapter title |
Crystallographic Analysis of MATE-Type Multidrug Exporter with Its Inhibitors
|
|---|---|
| Chapter number | 3 |
| Book title |
Bacterial Multidrug Exporters
|
| Published in |
Methods in molecular biology, January 2018
|
| DOI | 10.1007/978-1-4939-7454-2_3 |
| Pubmed ID | |
| Book ISBNs |
978-1-4939-7452-8, 978-1-4939-7454-2
|
| Authors |
Tsukasa Kusakizako, Yoshiki Tanaka, Christopher J. Hipolito, Hiroaki Suga, Osamu Nureki, Kusakizako, Tsukasa, Tanaka, Yoshiki, Hipolito, Christopher J., Suga, Hiroaki, Nureki, Osamu |
| Abstract |
Multidrug exporters expressed in pathogens efflux substrate drugs such as antibiotics, and thus, the development of inhibitors against them has eagerly been anticipated. Furthermore, the crystal structures of multidrug exporters with their inhibitors provide novel insights into the inhibitory mechanism and the development of more specific and effective inhibitors. We previously reported the complex structures of the Multidrug And Toxic compound Extrusion (MATE)-type multidrug exporter with the macrocyclic peptides, which inhibit the efflux of substrates by the MATE-type multidrug exporter (Tanaka et al., Nature 496:247-251, 2013). In this chapter, we describe methodologies of the screening and synthesis of macrocyclic peptides as inhibitors, as well as the purification, crystallization, and structure determination of the complexes of the MATE-type multidrug exporter with its inhibitors. |
X Demographics
Geographical breakdown
| Country | Count | As % |
|---|---|---|
| Unknown | 3 | 100% |
Demographic breakdown
| Type | Count | As % |
|---|---|---|
| Members of the public | 2 | 67% |
| Scientists | 1 | 33% |
Mendeley readers
Geographical breakdown
| Country | Count | As % |
|---|---|---|
| Unknown | 10 | 100% |
Demographic breakdown
| Readers by professional status | Count | As % |
|---|---|---|
| Student > Ph. D. Student | 4 | 40% |
| Other | 2 | 20% |
| Student > Bachelor | 1 | 10% |
| Researcher | 1 | 10% |
| Student > Postgraduate | 1 | 10% |
| Other | 0 | 0% |
| Unknown | 1 | 10% |
| Readers by discipline | Count | As % |
|---|---|---|
| Biochemistry, Genetics and Molecular Biology | 4 | 40% |
| Chemistry | 2 | 20% |
| Agricultural and Biological Sciences | 2 | 20% |
| Pharmacology, Toxicology and Pharmaceutical Science | 1 | 10% |
| Unknown | 1 | 10% |